Correlation study between A3 adenosine receptor binding affinity and anti-renal interstitial fibrosis activity of truncated adenosine derivatives
| Autor: | Ji-Youn Lee, Hunjoo Ha, Lak Shin Jeong, Dnyandev B. Jarhad, Chong-Woo Park, Gyudong Kim, Jinha Yu, Hyuk Woo Lee |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Chemistry Organic Chemistry Antagonist Pharmacology Inhibitory postsynaptic potential medicine.disease A3 adenosine receptor binding Adenosine 03 medical and health sciences Thionucleosides 030104 developmental biology 0302 clinical medicine Downregulation and upregulation 030220 oncology & carcinogenesis Drug Discovery medicine Renal fibrosis Molecular Medicine Kidney disease medicine.drug |
| Zdroj: | Archives of Pharmacal Research. 42:773-779 |
| ISSN: | 1976-3786 0253-6269 |
| Popis: | Truncated 4'-thionucleosides 1-4 and 4'-oxonucleosides 5-8 as potent and selective A3AR antagonists were synthesized from D-mannose and D-erythronic acid γ-lactone, respectively. These nucleosides were evaluated for their anti-fibrotic renoprotective activity in TGF-β1-treated murine proximal tubular (mProx) cells. Their antagonistic activities for A3AR were proportional to their inhibitory activities against TGF-β1-induced collagen I upregulation in mProx cells. This result suggests that the binding affinity of A3AR antagonists is closely correlated with their anti-fibrotic activity. Thus, A3AR antagonists might be novel therapeutic candidates for treating chronic kidney disease. |
| Databáze: | OpenAIRE |
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